ChEMBL ligand: CHEMBL236593 (Mk-0974, MK-0974, MK0974, Telcagepant)
Calcitonin gene-related peptide 1 in Human [ChEMBL: CHEMBL5293] [UniProtKB: P06881] Calcitonin gene-related peptide 1 in Rat [ChEMBL: CHEMBL5735] [UniProtKB: P01256] There should be some charts here, you may need to enable JavaScript!
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human [ChEMBL: CHEMBL2107838] [GtoPdb: 51, 47] [UniProtKB: O60894, Q16602] There should be some charts here, you may need to enable JavaScript!
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Human [ChEMBL: CHEMBL3798] [GtoPdb: 47] [UniProtKB: Q16602] There should be some charts here, you may need to enable JavaScript!
CGRP receptor in Human [GtoPdb: 48] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Calcitonin gene-related peptide 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5293] [UniProtKB: P06881]
ChEMBL	Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr	B	4	pKi	>100000	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
ChEMBL	Displacement of [125I]adrenomedullin form CGRP receptor in human SK-N-MC cell membrane by competitive binding assay	B	9.11	pKi	0.78	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
ChEMBL	Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr	B	8.66	pIC50	2.2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
Calcitonin gene-related peptide 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5735] [UniProtKB: P01256]
ChEMBL	Inhibition of rat CGRP	B	5.92	pKi	1200	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6705-6708 [PMID:21982500]
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2107838] [GtoPdb: 51, 47] [UniProtKB: O60894, Q16602]
ChEMBL	Inhibition of human CLR/RAMP1	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2020) 63: 6600-6623 [PMID:32058712]
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3798] [GtoPdb: 47] [UniProtKB: Q16602]
ChEMBL	Antagonist activity against CGRP receptor assessed as inhibition of CGRP-mediated vasorelaxation in human coronary arteries	B	8.43	pKd	3.71	nM	Kd	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Reversible saturable binding affinity to human CGRP receptor using [3H]-labeled compound	B	8.72	pKd	1.9	nM	Kd	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Displacement of [125I]-CGRP from human recombinant CGRP receptor	B	9.1	pKi	0.8	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2683-2686 [PMID:21251825]
ChEMBL	Displacement of [125I]human CGRP from human CLR expressed in HEK293 cells coexpressing human RAMP1	B	9.1	pKi	0.8	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4740-4742 [PMID:19577468]
ChEMBL	Displacement of [125I]human CGRP from human CLR expressed in HEK 293 cells coexpressing human RAMP1 after 3 hrs by scintillation counting	B	9.1	pKi	0.8	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6368-6372 [PMID:19818613]
ChEMBL	Displacement of [125I]CGPR from human CL receptor expressed in HEK293 cells	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2007) 50: 5564-5567 [PMID:17929795]
ChEMBL	Antagonist activity at human CGRP receptor	B	9.11	pKi	0.77	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3157-3161 [PMID:23632269]
ChEMBL	Displacement of [125I]-hCGRP from human CGRP receptor expressed in HEK293 cells	B	9.11	pKi	0.77	nM	Ki	ACS Med Chem Lett (2013) 4: 863-868 [PMID:24900761]
ChEMBL	Binding affinity to human CGRP receptor	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity against human CGRP receptor in presence of 50% human serum by cell based cAMP accumulation assay	F	7.96	pIC50	11	nM	IC50	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production in presence of 50% human serum	F	7.96	pIC50	11	nM	IC50	J Med Chem (2007) 50: 5564-5567 [PMID:17929795]
ChEMBL	Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay in presence of 50% human serum	F	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4740-4742 [PMID:19577468]
ChEMBL	Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins in presence of 50% human serum by scintillation proximity assay	F	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6368-6372 [PMID:19818613]
ChEMBL	Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay in presence of 50% human serum	F	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2683-2686 [PMID:21251825]
ChEMBL	Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 30 mins by scintillation proximity assay	F	8.62	pIC50	2.4	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4740-4742 [PMID:19577468]
ChEMBL	Antagonist activity against human CGRP receptor by cell based cAMP accumulation assay	F	8.66	pIC50	2.2	nM	IC50	J Med Chem (2014) 57: 7838-7858 [PMID:24960305]
ChEMBL	Antagonist activity at human CL receptor expressed in E10 cells assessed as CGRP-stimulated cAMP production	F	8.66	pIC50	2.2	nM	IC50	J Med Chem (2007) 50: 5564-5567 [PMID:17929795]
ChEMBL	Antagonist activity at CGRP receptor assessed as inhibition of CGRP-stimulated cAMP production by cell based assay	F	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2683-2686 [PMID:21251825]
ChEMBL	Antagonist activity at human CLR expressed in HEK293 cells coexpressing human RAMP1 assessed as inhibition of human CGRPalpha-induced cAMP production after 5 mins by scintillation proximity assay	F	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6368-6372 [PMID:19818613]
CGRP receptor in Human [GtoPdb: 48]
GtoPdb	-	-	9.1	pKi	-	-	-	J Pharmacol Exp Ther (2008) 324: 416-21 [PMID:18039958]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]